Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Equilibrium modeling of 5-HT2A receptors with [F-18]deuteroaltanserin and PET: Feasibility of a constant infusion paradigm
Autore:
van Dyck, CH; Soares, JC; Tan, PZ; Staley, JK; Baldwin, RM; Amici, LA; Fu, X; Garg, PK; Seibyl, JP; Charney, DS; Innis, RB;
Indirizzi:
Yale Univ, Sch Med, Dept Psychiat, New Haven, CT 06520 USA Yale Univ New Haven CT USA 06520 , Dept Psychiat, New Haven, CT 06520 USA Yale Univ, Sch Med, Dept Diagnost Radiol, New Haven, CT 06520 USA Yale Univ New Haven CT USA 06520 Diagnost Radiol, New Haven, CT 06520 USA VA Connecticut Healthcare, W Haven, CT USA VA Connecticut Healthcare W Haven CT USA cut Healthcare, W Haven, CT USA
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 8, volume: 27, anno: 2000,
pagine: 715 - 722
SICI:
0969-8051(200011)27:8<715:EMO5RW>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON-EMISSION-TOMOGRAPHY; F-18 ALTANSERIN; HUMAN-BRAIN; SUICIDE VICTIMS; ALZHEIMER-TYPE; BINDING-SITES; SEROTONIN RECEPTORS; REDUCED BINDING; FRONTAL-CORTEX; DEMENTIA;
Keywords:
[F-18]deuteroaltanserin; 5-HT2A receptor; serotonin; PET;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
44
Recensione:
Indirizzi per estratti:
Indirizzo: van Dyck, CH Yale Univ, Sch Med, Dept Psychiat, 333 Cedar St,CB 2041, New Haven, CT 06520 USA Yale Univ 333 Cedar St,CB 2041 New Haven CT USA 06520 520 USA
Citazione:
C.H. van Dyck et al., "Equilibrium modeling of 5-HT2A receptors with [F-18]deuteroaltanserin and PET: Feasibility of a constant infusion paradigm", NUCL MED BI, 27(8), 2000, pp. 715-722

Abstract

[F-18]Altanserin has emerged as a promising positron emission tomography (PET) ligand for serotonin-2A (5 HT2A) receptors. The deuterium substitutionof both of the 2'-hydrogens of altanserin ([F-18]deuteroaltanserin) yieldsa metabolically more stable radiotracer with higher ratios of parent tracer to radiometabolites and increased specific brain uptake than [F-18]altanserin. The slower metabolism of the deuterated analog might preclude the possibility of achieving stable plasma and brain activities with a bolus plus constant infusion within a reasonable time frame for an F-18-labeled tracer(T-1/2 110 min). Thus, the purpose of this study was to test the feasibility in human subjects of a constant infusion paradigm for equilibrium modeling of [F-18]deuteroaltanserin with PET. Seven healthy male subjects were injected with [F-18]deuteroaltanserin as a bolus plus constant infusion lasting 10 h postinjection. PET acquisitions and venous blood sampling were performed throughout the infusion period. Linear regression analysis revealed that time-activity curves for both specific brain uptake and plasma [F-18]deuteroaltanserin concentration stabilized after about 5 h, This permitted equilibrium modeling and estimation of V-3' (ratio of specific uptake to total plasma parent concentration) and the binding potential V-3 (ratio of specific uptake to free plasma parent concentration), Cortical/cerebellar ratios were increased by 26% relative to those we previously observed with [F-18]altanserin using similar methodology in a somewhat older subject sample. These results demonstrate feasibility of equilibrium imaging with [F-18]deuteroaltanserin and suggest that it may be superior to [F-18]altanserin as a PET radioligand. NUCL MED BIOL 27;8:715-722, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 09:08:35